Rosiglitazone maleate (Synonyms: BRL 49653C) |
| Catalog No.GC11318 |
A PPARγ agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 155141-29-0
Sample solution is provided at 25 µL, 10mM.
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Rosiglitazone maleate is the maleic acid salt form of rosiglitazone, a potent insulin sensitizer, which is used for the treatment of diabetes. Rosiglitazone belongs to a group of compounds, thiazolidinediones (TZDs), which selectively ligate the nuclear transcription factor peroxisome-proliferator-activated receptor-γ (PPARγ). As a TZD, rosiglitazone improves the sensitivity of end organs to insulin through PPARγ activation which poteniates them to lower concentrations of blood glucose. Despite of its beneficial effects of targeting insulin resistance, recent studies has shown that rosiglitazone is associated with several moderate to severe adverse effects, including hemodilution, anemia, weight gain, and edema as well as increased risk for heart failure and myocardial ischemic events.
Reference
[1].Andreas Pfutzner, Birgit Wilhelm, and Thomas Forst. Rosiglitazone and glimeperide: review of clinical results supporting a fixed dose conbination. Vascular Health and Risk Management 2007: 3(2) 211-220
[2].Adie Vilioen and Alan Sinclair. Safety and efficacy of rosiglitazone in the elderly diabetic patient. Vascular Health and Risk Management 2009:5 389-395
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Kinase experiment: |
cDNA encoding amino acids 174-475 of PPARγ1 is amplified via polymerase chain reaction and inserted into bacterial expression vector pGEX-2T. GST-PPARγ LBD is expressed in BL21(DE3)plysS cells and extracts. For saturation binding analysis, bacterial extracts (100 μg of protein) are incubated at 4°C for 3 h in buffer containing 10 mM Tris (pH 8.0), 50 mM KCl, 10 mM dithiothreitol with [3H]-BRL49653 (specific activity, 40 Ci/mmol) in the presence or absence of unlabeled Rosiglitazone. Bound is separated from free radioactivity by elution through 1-mL Sephadex G-25 desalting columns. Bound radioactivity eluted in the column void volume and is quantitated by liquid scintillation counting[1]. |
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Cell experiment: |
C3H10T1/2 cells are grown in a 24-well plate in DME medium supplemented with 10% fetal calf serum. Medium and compound (Rosiglitazone) are exchanged every 3 days. Cells are stained at day 7 with Oil Red O and photographed[1]. |
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Animal experiment: |
Rats are intravenously injected with 38 mg/kg streptozotocin and after 48 h, diabetes is identified by urinary glucosuria and then random blood sugar is measured and this day is regarded as day 0. Animals with a serum glucose level of 220-300 mg/dL are selected to be used in this study. Rats are randomly separated into five groups for daily drug administration for 8 weeks: group 1: control nondiabetic rats given a vehicle only (0.5 mL/kg of 0.5% carboxy methyl celleluse orally), group 2: control diabetic rats given a vehicle, group 3: diabetic rats receiving Rosiglitazone (5 mg/kg orally), group 4: diabetic rats receiving losartan (2 mg/kg, orally), and group 5: diabetic rats receiving both Rosiglitazone and losartan[2]. |
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References: [1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. |
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| Cas No. | 155141-29-0 | SDF | |
| Synonyms | BRL 49653C | ||
| Chemical Name | (Z)-but-2-enedioic acid;5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3.C(=CC(=O)O)C(=O)O | ||
| Formula | C18H19N3O3S.C4H4O4 | M.Wt | 473.5 |
| Solubility | ≥ 23.7 mg/mL in DMSO, ≥ 19 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1119 mL | 10.5597 mL | 21.1193 mL |
| 5 mM | 0.4224 mL | 2.1119 mL | 4.2239 mL |
| 10 mM | 0.2112 mL | 1.056 mL | 2.1119 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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